公开(公告)号：EP3177596B1

公开(公告)日：2018-04-18

申请号：EP16705789.2

申请日：2016-02-23

申请人： F.I.S.- Fabbrica Italiana Sintetici S.p.A.

发明人： ZARAMELLA, Simone ,  ROSSI, Emiliano ,  DE LUCCHI, Ottorino ,  SERAFINI, Siro

IPC分类号： C07D223/28

CPC分类号： C07D223/26 ,  B01J2231/643 ,  B01J2540/32 ,  C07D223/28

摘要： Object of the present invention is an improved process for the preparation of Elsicarbazepine and Eslicarbazepine acetate by means of chiral Ruthenium catalysts.

公开(公告)号：EP2421853A1

公开(公告)日：2012-02-29

申请号：EP09751896.3

申请日：2009-11-09

申请人： F.I.S. Fabbrica Italiana Sintetici S.p.A.

发明人： SERAFINI, Siro ,  CASTELLIN, Andrea ,  DAL SANTO, Claudio

IPC分类号： C07D403/06

CPC分类号： C07D403/06

摘要： The present invention refers to the synthesis of 3-{[(2R)-l-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-lH-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.

公开(公告)号：EP2046733A1

公开(公告)日：2009-04-15

申请号：EP06776610.5

申请日：2006-08-04

申请人： F.I.S. Fabbrica Italiana Sintetici S.p.A.

发明人： SERAFINI, Siro ,  MOTTERLE, Riccardo ,  BRASOLA, Elena

IPC分类号： C07C269/04 ,  C07D249/18

CPC分类号： C07C269/04 ,  C07D249/18 ,  C07C271/22

摘要： A process for the preparation of ω-alkoxycarbonylamino-α-aminoacids and α,ω orthogonally diprotected diaminoacids from α,ω-diaminoacids using 1- alkoxycarbonylbenzotriazoles as protecting agents is disclosed. In an alternative embodiment, carbamoylating agents in the presence of benzotriazoles are used instead of 1-alkoxycarbonylbenzotriazoles. This reaction is preferably applied to the preparation of ε- alkoxycarbonyllysines from lysine. A process for the preparation of t-butoxycarbonylbenzotriazoles and novel complexes of ω-alkoxycarbonylamino-α-aminoacids with benzotriazoles are also disclosed.

公开(公告)号：EP3177596A1

公开(公告)日：2017-06-14

申请号：EP16705789.2

申请日：2016-02-23

申请人： F.I.S.- Fabbrica Italiana Sintetici S.p.A.

发明人： ZARAMELLA, Simone ,  ROSSI, Emiliano ,  DE LUCCHI, Ottorino ,  SERAFINI, Siro

IPC分类号： C07D223/28

CPC分类号： C07D223/26 ,  B01J2231/643 ,  B01J2540/32 ,  C07D223/28

摘要： Object of the present invention is an improved process for the preparation of Elsicarbazepine and Eslicarbazepine acetate by means of chiral Ruthenium catalysts.

摘要翻译： 本发明的目的是通过手性钌催化剂制备乙酰卡巴酯和乙酸艾利卡西平的改进方法。

公开(公告)号：EP2421853B1

公开(公告)日：2013-07-24

申请号：EP09751896.3

申请日：2009-11-09

申请人： F.I.S.- Fabbrica Italiana Sintetici S.p.A.

发明人： SERAFINI, Siro ,  CASTELLIN, Andrea ,  DAL SANTO, Claudio

IPC分类号： C07D403/06

CPC分类号： C07D403/06

公开(公告)号：EP2046733B1

公开(公告)日：2011-10-05

申请号：EP06776610.5

申请日：2006-08-04

申请人： F.I.S. Fabbrica Italiana Sintetici S.p.A.

发明人： SERAFINI, Siro ,  MOTTERLE, Riccardo ,  BRASOLA, Elena

IPC分类号： C07C269/04 ,  C07D249/18

CPC分类号： C07C269/04 ,  C07D249/18 ,  C07C271/22

摘要： A process for the preparation of ω-alkoxycarbonylamino-α-aminoacids and α,ω orthogonally diprotected diaminoacids from α,ω-diaminoacids using 1- alkoxycarbonylbenzotriazoles as protecting agents is disclosed. In an alternative embodiment, carbamoylating agents in the presence of benzotriazoles are used instead of 1-alkoxycarbonylbenzotriazoles. This reaction is preferably applied to the preparation of ε- alkoxycarbonyllysines from lysine. A process for the preparation of t-butoxycarbonylbenzotriazoles and novel complexes of ω-alkoxycarbonylamino-α-aminoacids with benzotriazoles are also disclosed.